SULFONAMIDE ENDOTHELIN ANTAGONISTS

摘要

HA605a SULFONAMIDE ENDOTHELIN ANTAGONISTS Compounds of the formula inhibit endothelin, wherein: one of X and Y is N and the other is O; R is naphthyl or naphthyl substituted with R1, R2 and R3; R1, R2 and R3 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkanylalkyl, aryi, or aralkyl, any of which may be substituted with Z1, Z2 and Z3; halo; hydroxyl; cyano; nitro; -C(O)H; -C(O)R6; -C02H; -C02R6; -SH; -S(O)nR6; -S(O)m-OH; -S(O)m-OR6; -O-S(O)m-R6;-O-S(O)mOH; -O-S(O)m-OR6; -Z4-NR7R8; or-Z4-N(R11)-Z5-NR9R10; R4 and R5 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, oyclealkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl, any of which may be substituted with Z1, Z2 and Z3; halo; hydroxyl; cyano; nitro; -C(O)H; -C(O)R6; -CO2H; -CO2R6; -SH, -S(O)nR6;-S(O)m-OH; -S(O)m-OR6; -a S(O)m-R6;-O-S(O)mOH;-O-S(C)m-OR6; -Z4NR7R8;-Z4-N(R11)-Z5-NR9R10; or R4 and R5 together are alkylsne or alkenylene (either of which may be substituted with Z1, Z2 and Z3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached.